Smart phase transformation system based on lyotropic liquid crystalline@hard capsules for sustained release of hydrophilic and hydrophobic drugs

Abstract

Smart phase transformation systems@hard capsule (SPTS@hard capsule) based on lyotropic liquid crystalline (LLC) were developed for oral sustained release in this study. Doxycycline hydrochloride (DOXY) and meloxicam (MLX) were used as hydrophilic and hydrophobic model drug, respectively. Two systems were added with different additives, that is, gelucire 39/01, PEG 1000 and Tween 80 to adjust their melting point and release profiles. The phase transformation of these systems could be triggered by water as well as temperature. They could spontaneously transform into cubic phase or hexagonal phase when coming across with water, to achieve the 24 h sustained release profile. In addition, the obtained systems could switch between semisolid state and liquid state when temperature changed within room temperature and body temperature, which facilitated the phase transformation in gastrointestinal tract and during their encapsulation into hard capsules. LLC-based SPTS@hard capsule revealed potential for the industrialization of its oral administration on account of its drugs accommodation with different solubility, controllable release profile and simple preparation process.

Tamarillo Polyphenols Encapsulated-Cubosome: Formation, Characterization, Stability during Digestion and Application in Yoghurt

“…Similarly, reduction of the degradation in cubosome encapsulated bioactive antimicrobial peptide has been reported, showing resistance towards the enzymatic degradation [18]. Cubosomes have a high viscosity which hinders the diffusion of polyphenols into the release medium and slows the entry of water, which sustains the slow release profile [47]. The rate of release controlled by the structure also depends both on the partition coefficient and on the diffusion of the drug through the hydrocarbon tail region [48].…”

An intelligent phase transformation system based on lyotropic liquid crystals for sequential biomolecule delivery to enhance bone regeneration

“…And based on its internal structure of the lipid bilayer and water channel, the LCFS can provide a high capacity of hydrophilic/hydrophobic drug encapsulation. [22][23][24][25] Drugs will be located in these two different parts depending on their hydrophobicity and achieve a distinct release profile in one single drug delivery system. In addition, according to the in vitro release profile, DFO, as a pro-angiogenic molecule, could be released rapidly within 5 days while SIM, as a stimulator of endogenous BMP2, was sustainably released in a slow rate over weeks, suggesting a sequential presentation of these two bioactive molecules.…”

Cubosomal lipid nanoassemblies with pH-sensitive shells created by biopolymer complexes: A synchrotron SAXS study

“…Indeed, the gastrointestinal tract presents extreme pH variation to which drug delivery devices can be developed to respond in a manner to provide localized, optimized, and prolonged delivery of the carried bioactives. Regarding the cubosomes, the internal crystalline structure provides a complex crystalline network for the entrapment and encapsulation of hydrophobic and hydrophilic molecules [71]. With the intrinsic slow disassembling of the crystalline structure in biological media [14], the cubosomes may provide a prolonged release of the transported bioactives.…”